2. Epigenetics
  3. Epigenetic Reader Domain
  4. KMI169

KMI169 is a potent and selective inhibitor targeting lysine methyl-transferase (KMT9) (IC50 = 0.05 μM, Kd = 0.025 μM). KMI169 functions as a bi-substrate inhibitor targeting the cofactor S-5’-adenosyl-L-methionine (SAM) and substrate binding pockets of KMT9. KMI169 can downregulate target genes involved in cell cycle regulation and impair proliferation of tumor cells by inhibiting KMT9. KMI169 is a valuable tool to probe cellular KMT9 functions and can be research for combating diseases including prostate, lung, colon, and invasive bladder cancer.

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KMI169

KMI169 構造式

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 997 在庫あり
Solution
10 mM * 1 mL in DMSO USD 997 在庫あり
Solid
5 mg $750 在庫あり
10 mg $1250 在庫あり
25 mg $2750 在庫あり
50 mg $4500 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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KMI169 関連抗体

Top Publications Citing Use of Products

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Brd BRPF1 BRPF2 BRPF3 BRD2 BRD3 BRD4 BRDT CECR2 BD1 BD2 BRD7 BRD9 BET BAZ

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製品説明

KMI169 is a potent and selective inhibitor targeting lysine methyl-transferase (KMT9) (IC50 = 0.05 μM, Kd = 0.025 μM). KMI169 functions as a bi-substrate inhibitor targeting the cofactor S-5’-adenosyl-L-methionine (SAM) and substrate binding pockets of KMT9. KMI169 can downregulate target genes involved in cell cycle regulation and impair proliferation of tumor cells by inhibiting KMT9. KMI169 is a valuable tool to probe cellular KMT9 functions and can be research for combating diseases including prostate, lung, colon, and invasive bladder cancer[1][2].

IC50 & Target

KMT9[1]
体外実験

KMI169 (30 μM) only results in a 60% maximum inhibition against PRMT5, suggesting KMI169 does not target cellular PRMT5[1].
KMI169 (500 nM, 3 d) reduces the levels of H4K12mel, but does not alter histone markers such as H3K4me2, H3K9me2, and H4K20mel in PC-3M prostate tumor cells[1].
KMI169 (0.2-1 μM, 7 d) impairs proliferation of castration- and Enzalutamide (HY-70002)-resistant prostate cancer cell lines such as PC-3M, DU145, LNCaP-abl, and LNCaP-abl EnzaR, whereas proliferation of HepG2 and PANC-1 cells are not affected[1].
KMI169 (360 nM, 4 d) reduces mRNA levels for a selection of genes including MYB, AURKB, FOXA1, CDK2, BIRC5, E2F1, E2F8, CDC6, and LIG1[1].
KMI169 strongly reduces the proliferation of various cell lines such as J82 cells with a GI50 of 371 nM and RT-112 cells with a GI50 of 320 nM, as well as impairing proliferation of 5637, CAL-29, and UM-UC-3 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KMI169 関連抗体

Western Blot Analysis[1]

Cell Line: Prostate cancer cell lines PC-3M and LNCaP-abl
Concentration: 0.2-1 μM
Incubation Time: 7 d
Result: Revealed strong stabilization of endogenous KMT9.
Did not stabilize PRMT5 under the same conditions.
Strongly suppressed the proliferation of PC-3M cells with a GI50 of 150 nM.
分子量

604.53

分子式

C31H31Cl2N7O2
Appearance

Solid

Color

White to off-white

SMILES

NC1=C2C(C3=NN(C=C3Cl)CC4=CC=CC=C4)=CN([C@@H]5C[C@H](C6=CC(CN7CCC7)=CC=C6)[C@@H](O)[C@H]5O)C2=NC(Cl)=N1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (165.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6542 mL 8.2709 mL 16.5418 mL
5 mM 0.3308 mL 1.6542 mL 3.3084 mL
10 mM 0.1654 mL 0.8271 mL 1.6542 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6542 mL 8.2709 mL 16.5418 mL 41.3544 mL
5 mM 0.3308 mL 1.6542 mL 3.3084 mL 8.2709 mL
10 mM 0.1654 mL 0.8271 mL 1.6542 mL 4.1354 mL
15 mM 0.1103 mL 0.5514 mL 1.1028 mL 2.7570 mL
20 mM 0.0827 mL 0.4135 mL 0.8271 mL 2.0677 mL
25 mM 0.0662 mL 0.3308 mL 0.6617 mL 1.6542 mL
30 mM 0.0551 mL 0.2757 mL 0.5514 mL 1.3785 mL
40 mM 0.0414 mL 0.2068 mL 0.4135 mL 1.0339 mL
50 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8271 mL
60 mM 0.0276 mL 0.1378 mL 0.2757 mL 0.6892 mL
80 mM 0.0207 mL 0.1034 mL 0.2068 mL 0.5169 mL
100 mM 0.0165 mL 0.0827 mL 0.1654 mL 0.4135 mL
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KMI169 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KMI169KMI 169KMI-169Epigenetic Reader DomainProstate cancerSAMsubstrate binding pocketssmall molecule inhibitorcell cycle regulationcancerInhibitorinhibitorinhibit

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製品名:
KMI169
製品番号:
HY-157486
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